Trifluoroacetic acid → 3-[(4-Chlorophenyl)(cyclopropyl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indole

HRID 561675ノート

反応式

HRID 561675 の反応式
[CH:1]1([CH:4]([C:6]2[CH:11]=[CH:10][C:9]([Cl:12])=[CH:8][CH:7]=2)O)[CH2:3][CH2:2]1.FC(F)(F)C(O)=O.[F:20][C:21]1[CH:22]=[C:23]2[C:27](=[C:28]([CH2:30][S:31]([CH3:34])(=[O:33])=[O:32])[CH:29]=1)[NH:26][CH:25]=[CH:24]2>ClCCl>[Cl:12][C:9]1[CH:10]=[CH:11][C:6]([CH:4]([CH:1]2[CH2:3][CH2:2]2)[C:24]2[C:23]3[C:27](=[C:28]([CH2:30][S:31]([CH3:34])(=[O:32])=[O:33])[CH:29]=[C:21]([F:20])[CH:22]=3)[NH:26][CH:25]=2)=[CH:7][CH:8]=1

参加物

5

反応物 3

HCID 6422Trifluoroacetic acidHCID 866794-Chloro-alpha-cyclopropylbenzenemethanolHCID 583923185-Fluoro-7-[(methylsulfonyl)methyl]-1H-indole

生成物 1

HCID 583922023-[(4-Chlorophenyl)(cyclopropyl)methyl]-5-fluoro-7-[(methylsulfonyl)methyl]-1H-indole

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

64 mg (0.35 mmol) of the compound from Example 153A and 0.03 ml (0.42 mmol) of trifluoroacetic acid were added to 80 mg (0.35 mmol) of the compound from Example 87A in 2.5 ml of dichloromethane. The reaction mixture was stirred at RT for 45 min, the solvent was removed in vacuo, and the crude product was then purified by preparative HPLC (mobile phase: acetonitrile/water gradient). 110 mg (80% of theory) of the title compound were obtained.

後処理

  1. customthe solvent was removed in vacuo
  2. customthe crude product was then purified by preparative HPLC (mobile phase: acetonitrile/water gradient)

出典と根拠

ORDレコード
ord-7f26d019e75b41eca4de21487de82cf5
出典データセット
uspto-grants-2011_11
特許番号
US08063234B2

反応ノート

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